Concepedia

Lead Series Optimization

Lead Series Optimization is a pharmacokinetic optimization strategy that systematically refines a group of structurally related drug candidates to enhance their absorption, distribution, metabolism, excretion, and toxicity profiles while maintaining target activity.

78

Publications

4.5K

Citations

1.1K

Authors

129

Institutions

Publications per year

2017–2026

26

Parents

Publications

78

Structure Based Drug Design of Crizotinib (PF-02341066), a Potent and Selective Dual Inhibitor of Mesenchymal–Epithelial Transition Factor (c-MET) Kinase and Anaplastic Lymphoma Kinase (ALK)

J. Jean Cui, Michelle Tran‐Dubé, Hong Shen et al. · Journal of Medicinal Chemistry · 2011 · 922 citations · Full text

, , +17

Identification of <i>N</i>-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1<i>H</i>-pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment-Based X-Ray Crystallography and Structure Based Drug Design

Paul G. Wyatt, Andrew Woodhead, Valério Berdini et al. · Journal of Medicinal Chemistry · 2008 · 341 citations · Full text

, , +17

Lead Optimization of Aryl and Aralkyl Amine-Based Triazolopyrimidine Inhibitors of<i>Plasmodium falciparum</i>Dihydroorotate Dehydrogenase with Antimalarial Activity in Mice

Ramesh Gujjar, Farah El Mazouni, Karen L. White et al. · Journal of Medicinal Chemistry · 2011 · 167 citations · Full text

, , +17

Discovery of a Novel Warhead against β-Secretase through Fragment-Based Lead Generation

Stefan Geschwindner, Lise‐Lotte Olsson, Jeffrey S. Albert et al. · Journal of Medicinal Chemistry · 2007 · 148 citations · Full text

, , +16

Identification of Diaryl Ether-Based Ligands for Estrogen-Related Receptor α as Potential Antidiabetic Agents

Raymond J. Patch, Lily L. Searle, Alexander J. Kim et al. · Journal of Medicinal Chemistry · 2011 · 139 citations · Full text

, , +17

1–5 of 78

Authors

1.1K

  1. DR
    Daniel R. McMasters

    Merck & Co., Inc., Rahway, NJ, USA (United States), United States

    3 publications · 79 citations

    3

    h-index

  2. SA
    Susan A. Charman

    Monash University, Australia

    3 publications · 226 citations

    3

    h-index

  3. KL
    Karen L. White

    Monash University, Australia

    3 publications · 226 citations

    3

    h-index

  4. GZ
    Gaochao Zhou

    Merck & Co., Inc., Rahway, NJ, USA (United States), United States

    3 publications · 51 citations

    3

    h-index

  5. JG
    Jack Gibson

    Merck & Co., Inc., Rahway, NJ, USA (United States), United States

    3 publications · 51 citations

    3

    h-index

1–5 of 1.1K

Institutions

129

  1. Merck & Co., Inc., Rahway, NJ, USA (United States)

    Rahway, United States

    6 h-index

    150 publications

    4.1K citations

  2. GlaxoSmithKline (United Kingdom)

    London, United Kingdom

    4 h-index

    13 publications

    397 citations

  3. GlaxoSmithKline (Spain)

    Madrid, Spain

    3 h-index

    21 publications

    605 citations

  4. AstraZeneca (United Kingdom)

    Cambridge, United Kingdom

    3 h-index

    21 publications

    526 citations

  5. Swiss Tropical and Public Health Institute

    Allschwil, Switzerland

    3 h-index

    5 publications

    333 citations

  6. Medicines for Malaria Venture

    Geneva, Switzerland

    3 h-index

    11 publications

    1.2K citations

  7. University of Basel

    Basel, Switzerland

    3 h-index

    5 publications

    333 citations

  8. GlaxoSmithKline (Ireland)

    Cork, Ireland

    3 h-index

    30 publications

    705 citations

1–8 of 129

Venues

  1. Journal of Medicinal Chemistry

    39 publications · 3.2K citations

    25

    h-index

  2. ACS Medicinal Chemistry Letters

    9 publications · 247 citations

    9

    h-index

  3. Bioorganic & Medicinal Chemistry Letters

    4 publications · 107 citations

    4

    h-index

  4. ChemMedChem

    2 publications · 40 citations

    2

    h-index

  5. Molecular Pharmaceutics

    2 publications · 57 citations

    2

    h-index

1–5